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AR118982A1 - CYCLIC BRADYKININ RECEPTOR ANTAGONISTS - Google Patents

CYCLIC BRADYKININ RECEPTOR ANTAGONISTS

Info

Publication number
AR118982A1
AR118982A1 ARP200101443A ARP200101443A AR118982A1 AR 118982 A1 AR118982 A1 AR 118982A1 AR P200101443 A ARP200101443 A AR P200101443A AR P200101443 A ARP200101443 A AR P200101443A AR 118982 A1 AR118982 A1 AR 118982A1
Authority
AR
Argentina
Prior art keywords
group
substituted
halogen atom
alkyl
independently
Prior art date
Application number
ARP200101443A
Other languages
Spanish (es)
Inventor
Christoph Gibson
Joern Saupe
Horst Ambrosi
- Haustedt Lars Ole Dieter
Original Assignee
Pharvaris Gmbh
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Pharvaris Gmbh filed Critical Pharvaris Gmbh
Publication of AR118982A1 publication Critical patent/AR118982A1/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/16Otologicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Neurosurgery (AREA)
  • Endocrinology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Reproductive Health (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

La presente se refiere a un compuesto de acuerdo con la formula general (1), que actúa como un antagonista del receptor de bradiquinina (BK) B2; a una composición farmacéutica que contiene uno o más compuestos de la misma; a una preparación de combinación que contiene al menos un compuesto de la misma y al menos otro principio farmacéuticamente activo adicional; y a los usos de dicho(s) compuesto(s), incluido el uso como medicamento. Reivindicación 1: Un compuesto de fórmula general (1), o una de sus sales, en donde A representa un grupo seleccionado del grupo de fórmulas (2); A¹ es N o CH; A² es N o C-RA²; A³ es N o C-RA³; A⁴ es NH, O ó S; A⁵ es N-RA⁵; RA¹ representa un átomo de hidrógeno o un grupo metilo; cada uno de RA² y RA³, independientemente entre sí, representa un átomo de hidrógeno, un átomo de halógeno, OH, CN, NH₂; alquilo C₁₋₃, que puede estar sustituido con uno o más, grupo(s), idénticos o diferentes, seleccionados entre un átomo de halógeno, OH, =O y NH₂; alcoxi C₁₋₃, que puede estar sustituido con uno o más grupo(s), idénticos o diferentes, seleccionados entre un átomo de halógeno, OH, =O y NH₂; alcoxialquilo C₂₋₅, que puede estar sustituido con uno o más, grupo(s), idénticos o diferentes, seleccionados entre un átomo de halógeno, OH, =O y NH₂; C(O)NRA⁶RA⁷; o NRA⁶RA⁷; RA⁵, RA⁶ y RA⁷, cada uno independientemente entre sí, representa un átomo de hidrógeno o un grupo alquilo C₁₋₃, que puede estar sustituido con uno o más, grupo(s), idénticos o diferentes, seleccionados entre un átomo de halógeno, OH, =O y NH₂; R¹ representa un grupo alquilo C₁₋₃ o alcoxialquilo C₂₋₅, dicho grupo alquilo o alcoxialquilo puede estar sustituido con uno o más grupo(s), idénticos o diferentes, seleccionados entre un átomo de deuterio, un átomo de halógeno, OH, =O y NH₂; R² representa un átomo de hidrógeno o un átomo de deuterio; B representa un grupo heterocicloalquilo que contiene nitrógeno de 5 ó 6 miembros que tiene al menos un sustituyente oxo y n sustituyentes R, en donde n indica el número 0, 1, 2, 3, 4 ó 5; y cada R, en cada ocasión independientemente, representa un átomo de halógeno, OH, NRC¹RC², =O, G, OG o un grupo cicloalquilo C₃₋₅; cada uno de RC¹ y RC², independientemente entre sí, representan un átomo de hidrógeno o un grupo alquilo C₁₋₃; G representa un grupo alquilo C₁₋₆, en donde de 1 a 5 átomos de H pueden, en cada ocasión independientemente, estar sustituidos con un átomo de halógeno, =O, ORG¹ o NRG²RG³, y/o en donde un grupo CH₂, o dos grupos CH₂ no adyacentes, pueden estar sustituidos con O, C(O), OC(O), C(O)O, C(O)NH, NHC(O), NH, S, SO y/o SO₂; RG¹, RG² y RG³, cada uno independientemente entre sí, representan un átomo de hidrógeno, un grupo alquilo C₁₋₃, haloalquilo C₁₋₃, hidroxialquilo C₁₋₃, heteroalquilo C₁₋₃ o cicloalquilo C₃₋₅.The present relates to a compound according to the general formula (1), which acts as a bradykinin (BK) B2 receptor antagonist; to a pharmaceutical composition containing one or more compounds thereof; to a combination preparation containing at least one compound thereof and at least one additional pharmaceutically active ingredient; and to the uses of said compound(s), including use as a medicine. Claim 1: A compound of general formula (1), or one of its salts, wherein A represents a group selected from the group of formulas (2); A¹ is N or CH; A² is N or C-RA²; A³ is N or C-RA³; A⁴ is NH, O or S; A⁵ is N-RA⁵; RA¹ represents a hydrogen atom or a methyl group; each of RA² and RA³, independently of each other, represents a hydrogen atom, a halogen atom, OH, CN, NH₂; C₁₋₃ alkyl, which may be substituted with one or more identical or different group(s) selected from a halogen atom, OH, =O and NH₂; C₁₋₃ alkoxy, which may be substituted with one or more group(s), identical or different, selected from a halogen atom, OH, =O and NH₂; C₂₋₅ alkoxyalkyl, which may be substituted with one or more identical or different group(s) selected from a halogen atom, OH, =O and NH₂; C(O)NRA⁶RA⁷; or NRA⁶RA⁷; RA⁵, RA⁶ and RA⁷, each independently of one another, represents a hydrogen atom or a C₁₋₃ alkyl group, which may be substituted with one or more identical or different group(s) selected from a halogen atom, OH, =O and NH₂; R¹ represents a C₁₋₃ alkyl or C₂₋₅ alkoxyalkyl group, said alkyl or alkoxyalkyl group may be substituted with one or more group(s), identical or different, selected from a deuterium atom, a halogen atom, OH, = O and NH₂; R² represents a hydrogen atom or a deuterium atom; B represents a 5- or 6-membered nitrogen-containing heterocycloalkyl group having at least one oxo substituent and n R substituents, where n indicates the number 0, 1, 2, 3, 4 or 5; and each R, each time independently, represents a halogen atom, OH, NRC¹RC², =O, G, OG or a C₃₋₅ cycloalkyl group; each of RC¹ and RC², independently of each other, represents a hydrogen atom or a C₁₋₃ alkyl group; G represents a C₁₋₆ alkyl group, where from 1 to 5 H atoms may, on each occasion independently, be substituted by a halogen atom, =O, ORG¹ or NRG²RG³, and/or where a CH₂ group, or two non-adjacent CH₂ groups may be substituted with O, C(O), OC(O), C(O)O, C(O)NH, NHC(O), NH, S, SO and/or SO₂; RG¹, RG² and RG³ each independently of one another represent a hydrogen atom, a C₁₋₃ alkyl, C₁₋₃ haloalkyl, C₁₋₃ hydroxyalkyl, C₁₋₃ heteroalkyl or C₃₋₅ cycloalkyl group.

ARP200101443A 2019-05-23 2020-05-21 CYCLIC BRADYKININ RECEPTOR ANTAGONISTS AR118982A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP19176207 2019-05-23

Publications (1)

Publication Number Publication Date
AR118982A1 true AR118982A1 (en) 2021-11-17

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ID=66668713

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Country Status (13)

Country Link
US (1) US12312330B2 (en)
EP (1) EP3983402B1 (en)
JP (1) JP7462683B2 (en)
CN (1) CN113906018B (en)
AR (1) AR118982A1 (en)
AU (1) AU2020280924B2 (en)
CA (1) CA3139229A1 (en)
ES (1) ES2962971T3 (en)
MX (1) MX2021014288A (en)
PL (1) PL3983402T3 (en)
TW (1) TWI827847B (en)
UY (1) UY38706A (en)
WO (1) WO2020234479A1 (en)

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Also Published As

Publication number Publication date
AU2020280924A1 (en) 2021-11-25
US20220135542A1 (en) 2022-05-05
JP7462683B2 (en) 2024-04-05
TWI827847B (en) 2024-01-01
WO2020234479A1 (en) 2020-11-26
EP3983402C0 (en) 2023-08-16
TW202110429A (en) 2021-03-16
PL3983402T4 (en) 2024-04-02
CN113906018B (en) 2024-04-12
PL3983402T3 (en) 2024-04-02
US12312330B2 (en) 2025-05-27
EP3983402A1 (en) 2022-04-20
JP2022534389A (en) 2022-07-29
UY38706A (en) 2020-12-31
CN113906018A (en) 2022-01-07
AU2020280924B2 (en) 2023-07-27
ES2962971T3 (en) 2024-03-22
EP3983402B1 (en) 2023-08-16
MX2021014288A (en) 2022-01-06
CA3139229A1 (en) 2020-11-26

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